Drug reference

treprostinil

Prostacyclin Receptor Agonist / PGI2 analogue · Pulmonary Arterial Hypertension Agent

Prostacyclin Receptor Agonist / PGI2 analoguePulmonary Arterial Hypertension Agent

CDSCO approved

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

—

not curated

Top interactionssee all 12 →

AcalabrutinibSevereDatabaseDDInter
ApixabanSevereDatabaseDDInter
ArdeparinSevereDatabaseDDInter
AvapritinibSevereDatabaseDDInter

Mechanism

Treprostinil, a prostacyclin analogue, binds to the prostacyclin receptor (IPR) on PASMCs, activating the GS-AC-cAMP-PKA pathway. This leads to decreased cytosolic Ca2+ (via K+ channel activation and VDCC inhibition) and inhibition of myosin light chain kinase, resulting in smooth muscle relaxation and vasodilation. PKA also exerts antiproliferative effects.

Indications

PAHPH due to interstitial lung diseasesevere PAH (functional class IV)

Pharmacokinetics

Half-life

longer half-life than epoprostenol

Metabolism

Substrate for CYP2C8 and CYP2C9

Side effects

Common

pain (subcutaneous delivery)erythema (subcutaneous delivery)transient coughing (inhaled)jaw painhypotensionmyalgiaflushingnauseavomitingdizziness

Serious

oral treprostinil tablet shell can lodge in intestinal blind-end pouches and diverticula, possibly causing appendicitis and diverticulitis
inhibits platelet aggregation and increases the risk of bleeding